Overview Central & Peripheral Nervous System: 5-HT₄ receptor antagonists

References to Primarv Literaturess

• BRADLEY PB, ENGEL G, FENIUK W et al.: Proposals forthe classification and nomenclature of functional re-ceptors for 5-hydroxytryptamine. Neuropharmacol. (1986) 25:563–576.
   PubMed Web of Science ®Google Scholar
• SANGER GJ: Effects of metoclopramide and domperi-done on cholinergically-mediated contractions of hu-man isolated stomach muscle. J. Pharm. Pharmacol. (1985a) 37:661–664.
   PubMedGoogle Scholar
• BUCHHEIT KH, COSTELL B, ENGEL G et at 5-Hy-droxytryptamine receptor antagonism by metoclo-pramide and ICS 205–930 in the guinea-pig leads to enhancement of contractions of stomach muscle strips induced by electrical field stimulation and facilitation of gastric emptying in vivo. J. Phan,: Pharmacol. (1985) 37:664–667.
   Google Scholar
• SANGER GJ: Activation by metockopramide of a myen-teric 5-hydroxytryptamine-like receptor. J. Pharm. Phar-macol. (1987a) 39:449–453.
   PubMedGoogle Scholar
• SANGER GJ: Increased gut cholinergic activity and an-tagonism of 5-hydroxytryptamine M-receptors by BRL 24924: Potential clinical importance of BRL 24924. Br. J. Pharmacol. (19876) 91:77-87. Suggestion of a 5-HT-like action which was not mediated via 5-HT2 or 5-HT3 receptors.
   Google Scholar
• SANGER GJ: Three different ways in which 5-hy- droxytryptamine can affect cholinergic activity in guinea-pig isolated ileum. J. Pharm. Pharmacol. (1985b) 37:584–586.
   PubMedGoogle Scholar
• SANGER GJ, WARDLE KA: 5-Hydroxytryptaffulne, and cholinergic function in the gastrointestinal tract. In: Serotonin: From cell biology to pharmacology and therapeu- tics. Ed., PAOLETTI R, VANHOU1It PM, BRUNELLO N,MAGGI FM, DORDRECHT, KLUWER, pp 251–255. Further definition of 'atypical' responses to 5-HT.
   Google Scholar
• KING FD, HADLEY MS, JOINER KT et al.: Substituted benzamides with conformationally restricted side chains. 5. Azabicyclic [x.y.z.] derivatives as 5-HT4 recep-tor agonists and gastric motility stimulants. J. Med. Chem. (1993) 36:683–689.
   Google Scholar
• DUMUIS A, BOUHELAL R, SEBBEN M et at: Anon-classical 5-hydroxytryptamine receptor positively coupled with adenyiate cyclase in the central nervous system. Mol. Pharmacol. (1988) 34:880-887. Early definition of the S-HT4 receptor. See also 10 and 11.
   Google Scholar
• DUMUIS A, SEBBEN M, BOCKAERT J: The gastrointestinal prokinetic benzamine derivatives are agonists at thenon- classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons. Naunyn-Schmiedeberg's Arch. Pharmacol. (1989) 340:403–410.
   Google Scholar
• CRAIG DA, CLARKE DE: Pharmacological charac-terization of a neuronal receptor for 5-hyciroxytryp-tamine in guinea-pig ileum with properties similar to the 5-HT4 receptor. J. Pharm. Exp. Ther. (1990) 252:1378–1386.
   PubMed Web of Science ®Google Scholar
• CLARKE DE, CRAIG DA, FOZARD JR: The 5-HT4 receptor: naughty but nice. Trends Pharmacol. Sci. (1989) 10:385-386. An important early review. See also 13.
   Google Scholar
• BOCKAERT J, FOZARD JR, DUMUIS A, CLARKE DE: The 5-HT4 receptor: a place in the sun. Trends Pharmacol.Sci.(1992) 13:141–145.
   PubMed Web of Science ®Google Scholar
• FORD APDW, CLARKE DE: The 5-HT4 receptor. Med. Res. SoRev. (1993) 13:633-662. A comprehensive definition of the receptor.
   Google Scholar
• CRAIG DA, EGLEN RM, WALSH LKM, PERKINS LA, WHITING RL, CLARKE DE: 5-Methoxyirytarnine and 2-methyl-5-hy-droxytryptamine as a discriminative tool for the 5-HT3 and putative 5-HT4 receptors in guinea-pig ileum. Naunyn-Schmiedeberg's Arch. Pharmacol. (1990) 342:9–16.
   Google Scholar
• TONINI M, CANDURA SM, ONORI L, COCCINI T, MANZO L, RIZZI CA: 5-Hydroxytryptamine 4 receptor agonists facilitate cholinergic transmission in the circular mus-cle of guinea-pig ileum: Antagonism by tropisetron and DAU 6285. Life Sci. (1992) 50:PL173-PL178.
   Google Scholar
• ELSWWOD CJ, BUNCE KT, HUMPHREY PPA: Identification of putative 5-1IT4 receptors in guinea-pig ascendingcolon. Eur. J. Pharmacol, (1991) 196:149-155. A method of testing for functional activity at the receptor. See also 18 and 19.
   Google Scholar
• WARDLE KA, SANGER The guinea-pig distal colon A sensitive preparation for the investigation of 5-HT4receptor mediated contractions. Br. J. Pharmacol. (1993) 110:1593–1599.
   PubMedGoogle Scholar
• BAXTER GS, CRAIG DA, CLARKE DE: 5-Hydroxytryp-tamine 4 receptors mediate relaxation of rat oesophag-eal tunica muscularis mucosa. Naunyn- Schmiedeberg's Arch. Pharmacol. (1991) 343:439-446.25
   Google Scholar
• WALKAR MV, HEGDE SS, FORD APDW, CLARKE DE: Phar-macological analysis of endo-6-methoxy-8-methyl-8-az-abicyclo[3.2.1]oct-3-y1-2,3-dihydro-2-oxo-1H-benzhnid-azole-1-carboxylate hydrochloride (DAU 6285) at the 5-hydroxytryptamine 4 receptor in the tunica muscu-laris mucosae of rat esophagus and ileum of guinea-pig: role of endogenous 5-hydroxytryptamine. J. Pharm. Exp. Ther. (1993) 264:654–661.
   Google Scholar
• VILLALON CM, DEN BOER MO, HEILIGERS JPC, SAXENAPR: Mediation of 5-hydroxytryptamine-induced tachy-cardia in pig by the putative 5-HT4 receptor. Br. J. Pharrnacol. (1990) 100:665–667.
   Google Scholar
• KAUMANN AJ, SANDERS L, BROWN AM et al.: A 5-hy-droxytryptamine receptor in human atrium. Br.J. Phar-macol. (1990) 100:879–885.
   PubMed Web of Science ®Google Scholar
• DUMUIS A, GOZLAN H, SEBBEN M, CORY R, BOCKAERT Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285. Naunyn-Schmiedeberg's Arch. Pharmacol. (1992) 345:264. Definition of DAU 6285. See also 24.
   Google Scholar
• SCHIAVONE A, GIRALDO E, GIUDICI L, TURCONI M,SAGRADA A: DAU 6285: A novel antagonist at the puta-tive 5-HT4 receptor. Life Sci. (1992) 51:583–592.
   PubMedGoogle Scholar
• FLYNN DL, BECKER DP, MOORMANN AE et al.: New selective serotonin 5-HT4 receptor agonists and antago-nists (SC-53116, SC- 53606) based on a pyrrolizidine pharmacophore. Proc. 2nd Int. Symposium on Serotonin: Cell biology to pharmacology and therapeutics, USA (1992):48. Definition of SC-53116 and SC–53606.
   Google Scholar
• PARKER SG, HAMBURGERS, TAYLOR EM et al.: SB 203186,a potent 5-HT4 receptor antagonist, in porcine sinoa-trial node and human and porcine atrium. Br. J. Phar-macol. (1993) 108:68P.
   Google Scholar
• BUCHHEIT ICH, GAMSE R, PFANNKUCHE HJ: SDZ 205–557, a selective, surmountable antagonist for 5-HT4 recep-tors in the isolated guinea-pig ileum. Naunyn-Schmiede-betg's Arch. Pharmacol. (1992) 345:387-393. Definition of SDZ–205–557.
   Google Scholar
• EGLEN RM, ALVAREZ R, JOHNSON LG, LEUNG E, WONGEHF: The action of SDZ 205-557, at 5-hydroxytryp-tamine (5-HT3 and 5-IM) receptors. Br. J. Pharmacol. (1993) 108:376–382.
   PubMed Web of Science ®Google Scholar
• EGLEN RM, BONHAUS DW, CLARK R, HEGDE S, LEUNG E WHITING RL: RS-23597-190: A potent and selective 5-1IT4receptor antagonist. Br. J. Pharmacol. (1992) 107:439P Definition of RS–23597–190.
   Google Scholar
• GROSSMAN CJ, GALE JD, BUNCE KT et al.: Development of a radioligand binding assay for the 5-HT4 receptor:Use of a novel antagonist. Br. J. Pharmacol. (1993) 108:106P. A radioligand for the 5-HT4 receptor.
   Google Scholar
• WARDLE KA, ELLIS ES, GASTER LM et aLSB-204070 - A highly potent and selective 5-HT4 receptor antagonist.Br. J. Pharmacol. (1993) 10:15P. Definition of SB 204070.
   Google Scholar
• GROSSMAN CJ, KILPATRICK GJ, BUNCE KT: Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain. Br.J. Pharmacol. (1993) 109:618-624. A radioligand for the 5-HT4 receptor.
   Google Scholar
• BROWN AM, YOUNG TJ, PATCH TL et al: [1251I-SB 207710, a potent, selective radioligand for 5-HT4 receptors. Br.J. Pharmacol. (1993) 110:10P. SB 207710, a radioligand for the 5-HT4 receptor.
   Google Scholar
• LINNIK MD, BUTLER BT, MARTIN et al: Effect of ben-zamides on biochemical and motor responses at the 5-HT4 receptor in the guinea-pig ileum. FASEB (1991) Meeting proceedings: A1239.
   Google Scholar
• BLEY KR, EGLEN RM: Characterization of 5-hydroxytryp-taminergic depolarizations in the isolated rat vagus nerve. Br. J. Pharmacol. (1993) 108:246P. Characterization of the 5-HT4 receptor on the vagus nerve.
   Google Scholar
• GALZIN AM, DELAHAYE M: Interaction of forskolin with the 5-HT4 receptor mediated potentiation of twiches in guinea-pig ileum. Proc. 2nd Int. Symposium on Serotonin: from cell biology to pharmacology and therapeutics, USA (1992): 51.
   Google Scholar
• ANSANAY H, SEBBEN M, BOCKAERT J, DUMUIS A: Char-acterization of homologous 5-hydrox-ytryptamine 4 re-ceptor desensitization in colliculi neurons. Mol. Pharmacol. (1992) 42:808-816. The 5-HT4 receptor can only be desensitised by itself, not by other agents which increase adenylate cyclase activity.
   Google Scholar
• SANGER GJ, KING BF, WARDLE KA: 5-HT3 and 5-HT4 receptors in vomiting and gut movement. In: 5-Hy- droxytryptamine mechanisms in primary headaches. (1992) OLESEN J, SAXENA PR (Eds.). Raven press, NY pp 137–145. A long lasting, non-desensitising activity mediated via the 5-HT4 receptor.
   Google Scholar
• CIACCIA P, MAIO D, VACCA GF: An analytical short- and long-term model of presynaptic plasticity. Biol. Cy-bern.(1992) 67:335-345. A model of synaptic plasticity which may be relevant to an aspect of 5-HT4 receptor pharmacology within the enteric nervous system.
   Google Scholar
• VAN MEEL JCA, DLEDEREN W, HAIGH R et al.: The novel 5- HT4 receptor antagonist DAU 6285 antagonizes 5-hy-droxyttyptamine- induced tachycardia in pigs. Eur. J. Pharmacol. (1993) 233:295-297. Definition of DAU 6285 in vivo. See also 41.
   Google Scholar
• BINGHAM S, KING BF, RUSHANT B et al.: The 5-HT4 receptor antagonist SB 204070 inhibits the contractile response to 5-HT in the dog Heidenhain pouch. Br. J. Pharmacol. (1993) 110 :16P.
   Google Scholar
• BERMUDEZ J, DUNBAR A, SANGER GJ, TURNER DH: Stimu-lation of canine gastric motility by BRL 24924, a new gastric prokinetic agent. J. Gastrointestinal Motility (1990) 2:281–286.
   Google Scholar
• KAUMANN AJ, KING Fl), YOUNG RC.: Indazole as an indole bioisostere : 5-HT4 receptor antagonism. Bio. Chem. Med. Let. (1992) 2:419–420.
   Google Scholar
• FILE SE: The use of social interaction as a method for detecting anxiolytic activity of chlordiazepoxicle-like drugs. J.Neurosci. Methods (1980) 2:219–238.
   PubMed Web of Science ®Google Scholar
• SANGER GJ, KING FD: From metoclopramide to selective gut motility stimulants and 5-HT3 receptor antagonists. Drug Design & Delivery (1988) 3:273–295.
   PubMedGoogle Scholar
• MULLER-LISSNER S: Bavarian constipation study group: Treatment of chronic constipation with cisapride and placebo. Gut (1987) 28:1033.
   PubMed Web of Science ®Google Scholar
• BINNIE NR, CREASEY GH, EDMOND P, SMITH AN: The action of cisapride on the chronic constipation of paraplegia. Paraplegia (1988) 26:151–158.
   PubMedGoogle Scholar